Abstract: Processes are disclosed for making vortioxetine and pharmaceutically acceptable salts thereof. A propylene glycol solvate of vortioxetine hydrobromide is disclosed. A novel crystalline form of vortioxetine hydrobromide propylene glycol solvate, designated form AC1, is disclosed along with a method for making same. Form AC1 may be characterized by an x-ray powder diffraction pattern with peaks at about 19.64, 22.85, 25.51, 29.57, 30.18±0.2 degrees 2-theta.
Abstract: Disclosed herein are nitrogen-containing bicyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.
Type:
Grant
Filed:
May 24, 2017
Date of Patent:
December 24, 2019
Assignee:
Recurium IP Holdings, LLC
Inventors:
Kevin Duane Bunker, Peter Qinhua Huang, Sunny Abraham, Joseph Robert Pinchman, Chad Daniel Hopkins, Deborah Helen Slee
Abstract: The present invention relates to a compound of formula I, a stereoisomer, a prodrug, a pharmaceutically acceptable salt thereof or a pharmaceutically acceptable solvate thereof, and a process for preparing the same, a pharmaceutical composition comprising the same, and use of the compound in the preparation of medicine preventing and treating tumors, wherein the substituents are as defined in the specification.
Type:
Grant
Filed:
April 25, 2016
Date of Patent:
December 17, 2019
Assignee:
Xiamen University
Inventors:
Xianming Deng, Zhongji Zhuang, Zhou Deng, Xiaoxing Huang, Yan Liu, Ting Zhang, Wei Huang, Qingyan Xu, Zhiyu Hu
Abstract: Disclosed is a fused-ring or tricyclic aryl pyrimidine compound used as a mutation selectivity EGFR inhibitor. Specifically, disclosed is a compound represented by formula (I) and used as an EGFR inhibitor or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to a novel method of preparing copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride, to novel intermediate compounds, and to the use of said novel intermediate compounds for the preparation of said copanlisib, copanlisib dihydrochloride, or hydrates of copanlisib dihydrochloride. The present invention also relates to copanlisib dihydrochloride hydrates as compounds.
Type:
Grant
Filed:
November 5, 2015
Date of Patent:
December 3, 2019
Assignee:
Bayer Pharma Aktiengesellschaft
Inventors:
Jan-Georg Peters, Philipp Rubenbauer, Daniel Götz, Danja Großbach, Franz-Josef Mais, Heiko Schirmer, Juergen Stiehl, Kai Lovis, Andreas Lender, Martin Seyfried, Theodor Zweifel, Maurus Marty, Günter Weingärtner
Abstract: A regioselective one-step process for the synthesis of 2-hydroxyquinoxaline of Formula (1) or tautomers thereof: comprising reacting 1,2-phenylenediamine of Formula (2): with an excess amount of glyoxylic acid, glyoxylic acid monohydrate, or a 2,2-dialkoxyacetic acid of Formula (3): at a low temperature; wherein R1 and R2 are as defined in the specification.
Type:
Grant
Filed:
August 1, 2019
Date of Patent:
November 26, 2019
Assignee:
DEVELOPMENT CENTER FOR BIOTECHNOLOGY
Inventors:
Shao-Zheng Peng, Yuan-Ting Cho, Pao-Chiung Hong
Abstract: A compound of Formula (I), or a salt thereof, compositions comprising the compound, processes for its preparation and its use in therapy, for example in the treatment of parasitic diseases such as Chagas disease, Human African Trypanosomiasis (HAT), Animal African trypanosomiasis (AAT) and leishmaniasis, particularly visceral leishmaniasis (VL).
Type:
Grant
Filed:
August 3, 2016
Date of Patent:
November 19, 2019
Assignees:
GiaxoSmithKline Intellectual Property Development Limited, University of Dundee
Inventors:
Stephen Brand, Peter George Dodd, Eun Jung Ko, Maria Marco Martin, Timothy James Miles, Lars Henrik Sandberg, Michael George Thomas, Stephen Thompson
Abstract: The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.
Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.
Type:
Grant
Filed:
April 12, 2019
Date of Patent:
November 12, 2019
Assignee:
FORMA THERAPEUTICS, INC.
Inventors:
Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Mark J. Tebbe
Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.
Type:
Grant
Filed:
October 17, 2017
Date of Patent:
October 29, 2019
Assignee:
FORMA THERAPEUTICS, INC.
Inventors:
Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E.R. Schiller, Mark J. Tebbe
Abstract: The invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein the variables X, Y1—Y5, R1, R2, R3, R4, and Het have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Type:
Grant
Filed:
October 31, 2017
Date of Patent:
October 29, 2019
Assignees:
GENENTECH, INC., XENON PHARMACEUTICALS INC.
Inventors:
Daniel Sutherlin, Steven McKerrall, Michael Scott Wilson, Kwong Wah Lai, Philippe Bergeron, Birong Zhang, Ramsay Beveridge, Jean-Philippe Leclerc, Alexandre Lemire, Liang Zhao, Claudio Sturino
Abstract: The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes.
Type:
Grant
Filed:
April 19, 2019
Date of Patent:
October 22, 2019
Assignee:
FORMA THERAPEUTICS, INC.
Inventors:
Kenneth W. Bair, David R. Lancia, Jr., Hongbin Li, James Loch, Wei Lu, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Mark J. Tebbe
Abstract: Provided herein are modified amino acids comprising a tetrazine groups according to Formula I: polypeptides, antibodies, payloads and conjugates comprising these modified amino acid residues derived from the modified amino acids, and methods of producing the polypeptides, antibodies, payloads and conjugates comprising the modified amino acid residues. The polypeptides, antibodies, payloads and conjugates are useful in methods of treatment and prevention, methods of detection and methods of diagnosis.
Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
Type:
Grant
Filed:
May 4, 2018
Date of Patent:
October 15, 2019
Assignee:
Incyte Corporation
Inventors:
Yun-Long Li, Xiaozhao Wang, Chunhong He
Abstract: Azepine derivatives acting on 5-HT7 receptors and pharmaceutically acceptable salts thereof are disclosed. The azepine derivatives and the pharmaceutically acceptable salts thereof have high binding affinities for and high antagonistic activities on 5-HT7 receptors. Due to these advantages, the azepine derivatives and the pharmaceutically acceptable salts thereof can be applied to therapeutic or prophylactic agents for central nervous system diseases, such as depression, migraine, anxiety, pain, inflammatory pain, neuropathic pain, body temperature dysregulation, biorhythm dysregulation, sleep disturbance, and smooth muscle diseases where 5-HT7 receptors antagonistic activity is required.
Type:
Grant
Filed:
November 6, 2017
Date of Patent:
October 8, 2019
Assignee:
Korea Institute of Science and Technology
Inventors:
Hyunah Choo, Youngjae Kim, Jihye Seong, Ghil Soo Nam, Yong Seo Cho
Abstract: A reaction method comprising combining a carbonyl-substituted arylboronic acid or ester and an ?-effect amine in aqueous solution at a temperature between about ?5 C to 55 C, and a pH between 2 and 8 to produce an adduct. A process is also provided comprising: contacting a boron compound having a boron atom bonded to a sp2 hybridized carbon conjugated with a cis-carbonyl, the boron having at least one labile substituent, with an ?-effect amine, in a solvent for a time sufficient to form an adduct, which may proceed to further products.
Type:
Grant
Filed:
September 11, 2017
Date of Patent:
October 8, 2019
Assignee:
The Research Foundation for the State University o
Inventors:
Susan Bane Tuttle, Ozlem Dilek, Kamalika Mukherjee
Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof; processes for the preparation of; intermediates used in the preparation of; and compositions containing such compounds or salts, and their uses for treating D1-mediated (or D1-associated) disorders including, e.g., schizophrenia (e.g., its cognitive and negative symptoms), cognitive impairment (e.g., cognitive impairment associated with schizophrenia, AD, PD, or pharmacotherapy therapy), and Parkinson's disease.
Type:
Grant
Filed:
September 6, 2018
Date of Patent:
September 24, 2019
Assignee:
PFIZER INC.
Inventors:
Michael Aaron Brodney, Jennifer Elizabeth Davoren, Amy Beth Dounay, Ivan Viktorovich Efremov, David Lawrence Firman Gray, Michael Eric Green, Jaclyn Louise Henderson, Chewah Lee, Scot Richard Mente, Steven Victor O'Neil, Bruce Nelsen Rogers, Lei Zhang
Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
Type:
Grant
Filed:
December 28, 2017
Date of Patent:
September 24, 2019
Assignee:
ASTEX THERAPEUTICS LTD
Inventors:
Wim Vermeulen, Steven Anna Hostyn, Filip Albert Celine Cuyckens, Russell Mark Jones, Diego Fernando Domenico Broggini
Abstract: Provided is a highly potent and selective endocannabioid cellular reuptake inhibitor represented by formula (I): or a pharmaceutically acceptable solvate or co-crystal thereof as well as to a formulation comprising this inhibitor, and to methods of treatment in which this inhibitor is used.